Design, synthesis, pharmacological evaluation and molecular docking studies of substituted oxadiazolyl-2-oxoindolinylidene propane hydrazide derivatives

©2016 Sociedade Brasileira de Química. The manuscript describes design and synthesis of novel oxadiazolyl-2-oxoindolinylidene propane hydrazides as amide tethered hybrids of indole and oxadiazole and their evaluation for antiinflammatory and analgesic activity. The compounds were synthesized following five step reaction to yield fifteen derivatives as 3-(5-substituted-1,3,4-oxadiazol-2-yl)-N′-[2-oxo-1,2-dihydro-3Hindol-3-ylidene]propane hydrazides. The final derivatives 3-[5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-yl]-N′-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]propane hydrazide and 3-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]-N′-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]propane hydrazide were found to be highly promising molecules with severity index of 0.35 and 0.56, respectively, which is promising for an analgesic compound. The hydroxy and methyl substitution on phenyl ring system provided with active anti-inflammatory compounds having increase in reaction time of 84.11 and 83.17%, respectively compared to standard drug at 85.84%. Molecular docking studies exhibit comparable interaction with synthesized derivatives and standard drug having a dock score of -4.44 by the K-nearest neighbour genetic algorithm method.Published versio

Small interfering RNA for cancer treatment: overcoming hurdles in delivery

© 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences In many ways, cancer cells are different from healthy cells. A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy cells. Currently, nanotechnology-based delivery systems are the most promising tool to deliver DNA-based products to cancer cells. This review aims to highlight the latest development in the lipids and polymeric nanocarrier for siRNA delivery to the cancer cells. It also provides the necessary information about siRNA development and its mechanism of action. Overall, this review gives us a clear picture of lipid and polymer-based drug delivery systems, which in the future could form the base to translate the basic siRNA biology into siRNA-based cancer therapies

PRELIMINARY ANTICANCER ACTIVITY OF SOME PROP-2-ENEAMIDO, THIAZOLE AND 1-ACETYL-PYRAZOLIN DERIVATIVES OF AMINOBENZOTHIAZOLES

The scaffold 2-aminobenzothiazole fused with prop-2-eneamido, 1-acetyl-pyrazolin and thiazole moieties have been evaluated for their anticancer activity at the National Cancer Institute for testing against a panel of approximately 60 different human tumor cell lines derived from nine neoplastic cancer types. Relations between structure and activity are discussed, the most efficient anticancer compound (1) was found to be active with selective influence on renal cancer cell lines, especially on RXF 393 with a growth % of -71.40