DOI: 10.55522/jmpas.V11I6.4475
VOLUME 11 - ISSUE 6 NOVEMBER - DECEMBER 2022
Pravin Nandakumar Muli, Sonali Shankar Kamble, Sanjay Sudhakar Pekamwar, Balaji WamanraoMatore, Jagadish Singh, ParthaPratim Roy,Megha Mukund Muley, Bhaskar Sadashiv Dawane
School of Chemical Sciences, Swami Ramanand Teerth, Marathwada University, Nanded, Maharashtra, India
Refer this article
Bhaskar Sadashiv Dawane, Pravin Nandakumar Muli, Sonali Shankar Kamble, Sanjay Sudhakar Pekamwar, Balaji Wamanrao Matore, Jagadish Singh, ParthaPratim Roy, Megha Mukund Muley, 2022. Design, synthesis and evaluation of novel 3-(substitutedphenyl)-2-(4-(substitutedphenyl) thiazol-2-yl)-2h-pyrazolo [3, 4-d] thiazol-5(6h)-one derivatives as anti-breast cancer agents. Journal of medical pharmaceutical and allied sciences, V 11 - I 6, Pages - 5453 – 5460. Doi: 10.55522/jmpas.V11I6.4475.
ABSTRACT
Mainstream cancer research has continued to place a significant emphasis on the development of new and effective therapeutic candidates to tackle rising treatment resistance and off-target toxicities. Here, a series of novel 3-(substitutedphenyl)-2-(4-(substitutedphenyl)thiazol-2-yl)-2H-pyrazolo[3,4-d]thiazol-5(6H)-one derivatives were synthesized and characterized. The ability of the synthesized compounds to reduce the survival of the human breast cancer cell line MDA-MB 231 was evaluated. When compared to the reference chemical, 5-fluorouracil, 3-(4-chlorophenyl)-2-(4-(4-chlorophenyl)thiazol-2-yl)-2H-pyrazolo[3,4d]thiazol-5(6H)-oneand 3-(4-nitrophenyl)-2-(4-(4-nitrophenyl)thiazol-2-yl)-2H-pyrazolo[3,4d]thiazol-5(6H)-oneshowed the highest inhibitory activity (IC50:550 0.78 M and 504 0.89, respectively) on the viability of MDA-MB 231 cells. A molecular docking study has been carried out to discover more potent drugs.
Keywords:
Thiazolidione-2, 4-dione, Thiosemicarbazide, pyrazolo [3,4-d] thiazol-5(6H)-one, Anticancer activity, MDA-MB-231.