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Microwave‐Assisted Synthesis and Biological Evaluation of Some New Pyrazolothiazoles via a Multicomponent Approach
Author(s) -
Mamidala Srikanth,
Aravilli R Kowshik,
Vaarla Krishnaiah,
Vedula Rajeswar Rao
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201901633
Subject(s) - hela , in vitro , cell culture , chemistry , stereochemistry , neuroblastoma , furan , organic chemistry , biochemistry , biology , genetics
A series of new pyrazolothiazole hybrids were designed and synthesized by the microwave ‐ assisted multicomponent reaction of thiosemicarbazide, 3‐(furan‐2‐yl)‐1‐(pyridin‐2‐yl)prop‐2‐en‐1‐one and 1‐(pyridin‐2‐yl)‐3‐(thiophen‐2‐yl)prop‐2‐en‐1‐one with substituted 2‐bromoacetophenones. Structures of all the synthesized compounds were in good agreement with their spectral (FTIR, 1 H & 13 C NMR, Mass) and analytical data (CHN analysis). The target compounds were screened for their in vitro cytotoxic activity by testing against human adenocarcinoma (A549), cervical cancer (HeLa), human neuroblastoma (SK−N‐SH) and human prostate cancer (DU‐145) cell lines. From the in vitro results, it was found that the compound derived from p ‐ NO 2 phenyl ( 4 h) has potent activity against HeLa cell line with IC 50 value 9.97 ± 0.05 μM. Also, the compounds having p ‐OCH 3 phenyl ( 4 c) , phenyl ( 4 i) , and p ‐Cl phenyl ( 4 j) substitutions exhibited significant activity against HeLa cell line with IC 50 values 19.78 ± 0.03 μM, 18.47 ± 0.01 μM and 15.61 ± 0.06 μM respectively.