Papers by Chirag kumar J. Gohil
Asian Journal of Pharmaceutical and Clinical Research, 2021
Objective: Amide is one of the most important functional group presents in the chemicals, pharmac... more Objective: Amide is one of the most important functional group presents in the chemicals, pharmaceuticals, and foods. Conventionally, it has been synthesized from the carboxylic acid and amines. This conventional reaction is lengthy and involves hazardous chemicals and solvents. Hence, it poses waste management, solvent removal, and environmental issues to the industries. To overcome this limitation, we have reported the green chemistry-based method for the synthesis of amide from carboxylic acid and urea. Methods: In this reaction, we have used boric acid as a catalyst, it is a simple and readily available compound. It is simple, efficient, and solvent-free procedure which involves the trituration of the reactant mixture and subsequent, direct heating of the triturated mixture. Results: The rate of reaction is very high and can synthesize the amide quickly. Conclusion: Various amides were prepared in good yield by this technique.
Cancer is characterized by uncontrolled and abnormal cells growth. In the body, the cell growth a... more Cancer is characterized by uncontrolled and abnormal cells growth. In the body, the cell growth and cell<br> division are governing by apoptosis. The process of apoptosis is mainly regulated by the p53 protein. p53<br> is a tumor suppressor protein. The amount of p53 in a cell is mainly controlled by the negative regulator<br> murine double minute 2 (MDM2), which on complex formation with p53 leads to an overall reduction<br> of the p53 level. Inhibition of p53 function will inhibit the apoptosis and leads to cancer. Consequently,<br> inhibition of the MDM2/p53 interaction using the small molecules activates the p53 function and apoptosis<br> in the cells which contain the wild-type p53. It is a promising new therapeutic strategy for the treatment<br> of cancers retaining wild-type p53. However, the safety window of this class of compounds must be<br> evaluated. Moreover, it has to require the development of compounds, which can also b...
International Journal of Pharmaceutical Chemistry and Analysis, 2021
MDM2 inhibitors class of anti-neoplastic drugs has been evolve after the successful discovery of ... more MDM2 inhibitors class of anti-neoplastic drugs has been evolve after the successful discovery of the nutlins and other potent inhibitors. MDM2 inhibitors can specifically target the tumour cells in the body, by selectively reactivating the inhibited p53 function in the tumour cells.None of the compound of this class has been entered into the market till date, all are under clinical trials. Hence, various researcher classifies them according to their p53 topology mimetic property and as per their peptide type or non-peptide type.Synthetic peptide type of inhibitors can mimic the conformation of p53 helix. Whereas, small organic molecule (non-peptide) type of MDM2 inhibitors have been further subdivided as Non α-helix mimetics (small molecule inhibitors) and α-helix mimetics. In a line with synthetic inhibitors, many potent MDM2 inhibitors are derived from the natural origin (marine, fungus). Therefore, keeping in a view of all these characteristics, here we have classified them as pe...
Cancer is characterized by uncontrolled and abnormal cells growth. In the body, the cell growth a... more Cancer is characterized by uncontrolled and abnormal cells growth. In the body, the cell growth and cell division are governing by apoptosis. The process of apoptosis is mainly regulated by the p53 protein. p53 is a tumor suppressor protein. The amount of p53 in a cell is mainly controlled by the negative regulator murine double minute 2 (MDM2), which on complex formation with p53 leads to an overall reduction of the p53 level. Inhibition of p53 function will inhibit the apoptosis and leads to cancer. Consequently, inhibition of the MDM2/p53 interaction using the small molecules activates the p53 function and apoptosis in the cells which contain the wild-type p53. It is a promising new therapeutic strategy for the treatment of cancers retaining wild-type p53. However, the safety window of this class of compounds must be evaluated. Moreover, it has to require the development of compounds, which can also be able to target the cells which contain the mutated or deleted p53.
Cancer is a class of diseases characterized by out-of-control cell growth. There are so many type... more Cancer is a class of diseases characterized by out-of-control cell growth. There are so many types of cancer. In case of Women, Breast Cancer ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer. In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications. We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile pha...
Cancer is the biggest question-mark for the medical science. However many effective drugs are ava... more Cancer is the biggest question-mark for the medical science. However many effective drugs are available for the cancer treatment, the biggest obstacle is the selective targeting the drug to the cancer cells. Boron Neutron Capture Therapy(BNCT) is a selective therapy of the cancer, it may not affect or affect little to the normal cells, It works on 2 principles -(1)Boron can capture the neutron & getting unstable. (2) Subsequently nuclear fission of boron occurs via emitting radiation. So, Delivered the required dose of boron to the cancerous cells and triggering it with the Neutron beam to this cancer cells which contain the boron, This neutron is capture by the neutron of cancer cells, getting unstable & subsequently nuclear fission is occur, this lethal radiation ultimately kills the cancer cells & normal cells are survive. The nuclear reaction is: 10 B + nth → [ 11 B] → α + 7 Li + 2.31 MeV The future prospective are to limit the radiation to the cancer cells only & efficiently deliver the Boron to the cancer cell only, also evaluate the other radioactive materials like Gadolinium in place of Boron.
Journal of Analytical & Pharmaceutical Research
The generation of induced pluripotent stem cell (iPSC) from somatic cells demonstrated that matur... more The generation of induced pluripotent stem cell (iPSC) from somatic cells demonstrated that mature mammalian cells can be reprogrammed to a pluripotent state by the enforced expression of few embryogenic transcription factor. iPSCs are reprogrammed from human somatic cells through ectopic expression of various transcription factors viz. Oct4, Sox2, Klf4, and c-Myc (OSKM). This novel technology enables derivation of patient specific cells, which possess a potential cure for many diseases. In addition, iPSC technology has provided researchers with a unique tool to derive disease-specific stem cells for the study and possible treatment of cancer and also the degenerative disorders with autologous cells. Many cancer cells exchange with these cells and cure the cancer. We summarize in this article the potential clinical application of iPSC.
International Journal of Pharmaceutical Chemistry and Analysis, 2016
The chemical reaction which is occur by the absorption of the light or photon is called as Photoc... more The chemical reaction which is occur by the absorption of the light or photon is called as Photochemical reaction. And the branch of the chemistry which is dealing with the study of these types of reactions is called as photochemistry. Photochemical reaction are also called as light reaction, because they have got the activation energy from the light. In this article we have covered the important aspects of photochemistry. Like the various rules of photochemistry which are the base of photochemical reaction and the important phenomena Jablonski Diagram which states about the mechanism of photochemical reaction and various light radiation process which are happened by the electronic transitions. We have also discussed the Quantum Yield by which we can determine about the number of molecules activated or decomposed by absorption of single photon. Including the Quantum Efficiency which gives the description about the efficiency of the Photosensitive Devices and also with the types of photochemical reaction with examples, which gives the idea about the various chemical reaction which are types of photochemical reactions.
International Journal of Pharmaceutical Chemistry and Analysis
Cancer is a tumorous disease, which involves the unwanted cell growth and cell division. The imba... more Cancer is a tumorous disease, which involves the unwanted cell growth and cell division. The imbalance or inactivity of the apoptosis in the body is responsible for the occurrence of tumour and cancer. This apoptosis is regulated by the p53 protein, which is tumour suppressor protein. In the cancer cells, this p53 has been inhibited by the MDM2 protein. MDM2 interact with the p53 and make it inactive. This p53-MDM2 interaction is responsible for the cancer genesis. If we target this interaction, then we can initiate the apoptosis in the cancer cells by making the free p53 protein. There are many strategies to inhibit this p53-MDM2 interaction. Among them non-peptidic small molecule inhibitors are the convenient approach. Small molecule inhibitors have a three pocket binding, so they bind with p53 binding pocket (Trp 23, Leu 26 and Phe 19), present in the MDM2 protein. That is how it spares the p53 protein and makes it available in the cancer cells. Hence, small molecule inhibitors successfully inhibit the p53-MDM2 interaction and can initiate the apoptosis in the cancer cells, which are having the un-mutated p53 protein. They can't inhibit this interaction in the cells which contains the mutated or deleted p53 protein. Hence, this limitation must be addressed. Many of the small molecular MDM2 inhibitors have been successfully entered into the clinical trials and they are performing well. The clinical data indicate that the small molecular MDM2 inhibitors are having very low toxicity to the normal cells. And they are non-genotoxic so they are near to nontoxic to the normal cells. But none of the any small molecule MDM2 inhibitor has been enters into the market yet. So till then, it has required advancement and research to make more selective and specific for the cancer cells over the normal cells.
IP innovative publication pvt ltd, 2019
Cancer is a tumorous disease, which involves the unwanted cell growth and cell division. The imba... more Cancer is a tumorous disease, which involves the unwanted cell growth and cell division. The imbalance or inactivity of the apoptosis in the body is responsible for the occurrence of tumour and cancer. This apoptosis is regulated by the p53 protein, which is tumour suppressor protein. In the cancer cells, this p53 has been inhibited by the MDM2 protein. MDM2 interact with the p53 and make it inactive. This p53-MDM2 interaction is responsible for the cancer genesis. If we target this interaction, then we can initiate the apoptosis in the cancer cells by making the free p53 protein. There are many strategies to inhibit this p53-MDM2 interaction. Among them non-peptidic small molecule inhibitors are the convenient approach. Small molecule inhibitors have a three pocket binding, so they bind with p53 binding pocket (Trp 23, Leu 26 and Phe 19), present in the MDM2 protein. That is how it spares the p53 protein and makes it available in the cancer cells. Hence, small molecule inhibitors successfully inhibit the p53-MDM2 interaction and can initiate the apoptosis in the cancer cells, which are having the un-mutated p53 protein. They can’t inhibit this interaction in the cells which contains the mutated or deleted p53 protein. Hence, this limitation must be addressed. Many of the small molecular MDM2 inhibitors have been successfully entered into the clinical trials and they are performing well. The clinical data indicate that the small molecular MDM2 inhibitors are having very low toxicity to the normal cells. And they are non-genotoxic so they are near to nontoxic to the normal cells. But none of the any small molecule MDM2 inhibitor has been enters into the market yet. So till then, it has required advancement and research to make more selective and specific for the cancer cells over the normal cells.
The chemical reaction which is occur by the absorption of the light or photon is called as Photoc... more The chemical reaction which is occur by the absorption of the light or photon is called as Photochemical reaction. And the branch of the chemistry which is dealing with the study of these types of reactions is called as photochemistry. Photochemical reaction are also called as light reaction, because they have got the activation energy from the light. In this article we have covered the important aspects of photochemistry. Like the various rules of photochemistry which are the base of photochemical reaction and the important phenomena Jablonski Diagram which states about the mechanism of photochemical reaction and various light radiation process which are happened by the electronic transitions. We have also discussed the Quantum Yield by which we can determine about the number of molecules activated or decomposed by absorption of single photon. Including the Quantum Efficiency which gives the description about the efficiency of the Photosensitive Devices and also with the types of photochemical reaction with examples, which gives the idea about the various chemical reaction which are types of photochemical reactions.
Cancer is a class of diseases characterized by out-of-control cell growth. There are so many type... more Cancer is a class of diseases characterized by out-of-control cell growth. There are so many types of cancer. In case of Women, Breast Cancer ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer.
In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications.
We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile phase. The Rf values were compared and the Melting Point of the derivatives was determined. It was found that they were different from each others. Further, these derivatives were characterized and confirmed by IR, 1H-NMR, 13C-NMR and Mass Spectral Studies. For Anticancer activity, the selected compounds were submitted to National Cancer Institute (NCI) for in vitro anticancer assay and were evaluated for their anticancer activity. Primary in vitro dose anticancer assay was performed in full NCI 60 Cell panel in accordance with the protocol of the NCI, USA. Compound 1 has a 73.7 % and Compound 4 has a 52.56 % growth Inhibition of Breast Cancer cell lines
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Papers by Chirag kumar J. Gohil
In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications.
We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile phase. The Rf values were compared and the Melting Point of the derivatives was determined. It was found that they were different from each others. Further, these derivatives were characterized and confirmed by IR, 1H-NMR, 13C-NMR and Mass Spectral Studies. For Anticancer activity, the selected compounds were submitted to National Cancer Institute (NCI) for in vitro anticancer assay and were evaluated for their anticancer activity. Primary in vitro dose anticancer assay was performed in full NCI 60 Cell panel in accordance with the protocol of the NCI, USA. Compound 1 has a 73.7 % and Compound 4 has a 52.56 % growth Inhibition of Breast Cancer cell lines
In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications.
We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile phase. The Rf values were compared and the Melting Point of the derivatives was determined. It was found that they were different from each others. Further, these derivatives were characterized and confirmed by IR, 1H-NMR, 13C-NMR and Mass Spectral Studies. For Anticancer activity, the selected compounds were submitted to National Cancer Institute (NCI) for in vitro anticancer assay and were evaluated for their anticancer activity. Primary in vitro dose anticancer assay was performed in full NCI 60 Cell panel in accordance with the protocol of the NCI, USA. Compound 1 has a 73.7 % and Compound 4 has a 52.56 % growth Inhibition of Breast Cancer cell lines