Synthesis, Characterization, and Evaluation of Cytotoxic Effects of Novel Hybrid Steroidal Heterocycles as PEG Based Nanoparticles

Synthesis, Characterization, and Evaluation of Cytotoxic Effects of Novel Hybrid Steroidal Heterocycles as PEG Based Nanoparticles

Asian Pac J Cancer Prev. 2017 07 27;18(7):1937-1946

Authors: Abd Elhalim MM, Ismail NSM, M Yahya SM, Omar YY, Abd Rabou AA, Lasheen DS, Zawrah MF, Elmegeed GA

Abstract
Anticancer agents featuring hybrid molecules can improve effectiveness and diminish drug resistance. The current study aimed to introduce newly synthesized heterocyclic steroids of promising anticancer effects loaded in polyethylene glycol (PEG)•based nanoparticles form. Several heterocyclic steroids (1-9) were synthesized via multicomponent reactions (MCRs) and confirmed via the analytical and spectral data. Compounds 1, 2, 3, 4, 5, 6, 7 and 9, were investigated individually in their free and PEG based nano-size hybrid forms as anticancer agents against three human cell lines: hepatocellular carcinoma cells (HepG2); breast cancer cells (MCF-7); and colon cancer cells (HCT116). The neutral red supravital dye uptake assay was employed. Compound 6 in its PEG based nano-size form exhibited the best cytotoxic effects against HepG2 and HCT116 cell lines, with IC50 values of 2.44 μmol/l and 2.59 μmol/l, respectively. In addition, it demonstrated a low IC50 value against MCF-7 (3.46μmol/l) cells. This study introduced promising anticancer agents acting through conversion into PEG-based nanoparticles.

PMID: 28749624 [PubMed - as supplied by publisher]

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