Synthesis, cytotoxicity, and molecular docking of substituted 3-(2-methylbenzofuran-3-yl)-5-(phenoxymethyl)-1,2,4-oxadiazoles.

A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell lines. Compounds 6a (IC : 9.

Synthesis and cytotoxicity of novel 14α--(andrographolide-3-subsitutedisoxazole-5-carboxylate) derivatives.

Simple and efficient method was established for the synthesis of a new family of 14α--(andrographolide-3-subsitutedisoxazole-5-carboxylate) derivatives () from naturally occurring andrographolide () by selective esterification with propiolic acid at C-14 using protection and deprotection strategy followed by metal free 1,3-dipolar cycloaddition with aryl nitrile oxides. All the synthesised derivatives were tested for their cytotoxicity against HCT-15, HeLa and DU145 cell lines. Most of the compounds exhibited improved cytotoxic activity compared to the parent molecule andrographolide (), as the compounds , , , , and showed significant cytotoxicity against three cancer cell lines.

Synthesis and cytotoxicity of novel 14α--(1,4-disubstituted-1,2,3-triazolyl) ester derivatives of andrographolide.

A series of novel 14α--(1,4-disubstituted-1,2,3-triazolyl) ester derivatives of andrographolide (-) were synthesized from andrographolide (). For this endeavour, selective esterification at C-14 hydroxyl group of andrographolide () with propiolic acid protection, deprotection strategy followed by 1,4-regioselective [1,3]dipolar cycloaddition of alkyne, azide using Cu(I) catalyzed Click chemistry. All the synthesized derivatives were screened for their cytotoxicity on HCT-15, HeLa and K562 cell lines.