title: Synthesis and cytotoxic evaluation of novel 3-substituted derivatives of 2-indolinone.
abstract: The assessment of the degree or rate of cellular proliferation and cell viability is critical for the assessment of the effects of drugs on both normal and malignant cell populations. In the present study, a few novel 3-substituted derivatives of 2-indolinones were synthesized by condensation of substituted oxindole or isatin derivatives with appropriate aldehydes or primary aromatic amines respectively. The synthesized compounds were screened for their cytotoxicity against HT-29 (human colon adenocarcinoma cell line) and MCF-7 (human breast adenocarcinoma cell line) cells using short term cytotoxicity MTT assay protocol. A few derivatives with IC50 < 10 µM were identified among them. he compound bearing 5-bromo substitution was the most potent derivative. Global physicochemical properties for compounds IVa-e and Va-h were calculated and the two most active compounds (IVa and IVb) showed similar CLogP values.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. ; Student Research Committee, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors.forename: Shaya
authors.initials: S
authors.lastname: Mokhtari
authors.forename: Mahmoud
authors.initials: M
authors.lastname: Mosaddegh
authors.forename: Maryam
authors.initials: M
authors.lastname: Hamzeloo Moghadam
authors.forename: Zohreh
authors.initials: Z
authors.lastname: Soleymani
authors.forename: Saeideh
authors.initials: S
authors.lastname: Ghafari
authors.forename: Farzad
authors.initials: F
authors.lastname: Kobarfard
keywords: 3- substituted derivatives of 2-indolinones; Colon and breast cancer; Cytotoxicity; Indole derivatives; MTT assay