title: Gallic acid based steroidal phenstatin analogues for selective targeting of breast cancer cells through inhibiting tubulin polymerization.
abstract: Phenstatin analogues were synthesized on steroidal framework, for selective targeting of breast cancer cells. These analogues were evaluated for anticancer efficacy against breast cancer cell lines. Analogues 12 and 19 exhibited significant anticancer activity against MCF-7, hormone dependent breast cancer cell line. While analogues 10-14 exhibited significant anticancer activity against MDA-MB-231, hormone independent breast cancer cell line. Compound 10 showed significant oestrogen antagonistic activities with low agonistic activity in in vivo rat model. These analogues also retain tubulin polymerization inhibition activity. The most active analogue 10 was found to be non-toxic in Swiss albino mice up to 300 mg/kg dose. Gallic acid based phenstatin analogues may further be optimized as selective anti-breast cancer agents.
authors.affiliation: Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Lucknow, UP, India.
authors.forename: Swati
authors.initials: S
authors.lastname: Parihar
authors.forename: Atul
authors.initials: A
authors.lastname: Gupta
authors.forename: Amit K
authors.initials: AK
authors.lastname: Chaturvedi
authors.forename: Jyoti
authors.initials: J
authors.lastname: Agarwal
authors.forename: Suaib
authors.initials: S
authors.lastname: Luqman
authors.forename: Bendangla
authors.initials: B
authors.lastname: Changkija
authors.forename: Murli
authors.initials: M
authors.lastname: Manohar
authors.forename: Debabrata
authors.initials: D
authors.lastname: Chanda
authors.forename: C S
authors.initials: CS
authors.lastname: Chanotiya
authors.forename: Karuna
authors.initials: K
authors.lastname: Shanker
authors.forename: Anila
authors.initials: A
authors.lastname: Dwivedi
authors.forename: Rituraj
authors.initials: R
authors.lastname: Konwar
authors.forename: Arvind S
authors.initials: AS
authors.lastname: Negi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism*; D045744:Cell Line, Tumor; D005260:Female; D005707:Gallic Acid / Q000737:chemistry*; D006801:Humans; D058105:Polymerization / Q000187:drug effects*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014404:Tubulin / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D014404:Tubulin; D005707:Gallic Acid