title: The first total synthesis and biological evaluation of marine natural products ma'edamines A and B.
abstract: We have developed the first total syntheses of marine natural products ma'edamines A (18) and B (20). Structurally, they contain a pyrazine-2-(1H)-one core and were screened for antiproliferative activity on several cancer cell lines. Out of the six cell lines tested, ma'edamines A and B showed significant cytotoxicity against human colon cancer line COLO 205 (IC(50) 7.9 and 10.3 μM, respectively), breast cancer cell line MCF-7 (IC(50): 6.9 and 10.5 μM, respectively) and human lung adenocarcinoma cell line A549 (IC(50): 12.2 and 15.4 μM, respectively). The apoptotic effect of ma'edamines was confirmed by comet assay. Hence ma'edamines are likely to be useful as leads for development of a new class of anti-cancer agents.
authors.affiliation: GVK Biosciences Private Limited, Medicinal Chemistry Division, 28A, IDA Nacharam, Hyderabad 500076, India.
authors.forename: Sanjay
authors.initials: S
authors.lastname: Saha
authors.forename: Ch
authors.initials: Ch
authors.lastname: Venkata Ramana Reddy
authors.forename: T
authors.initials: T
authors.lastname: Chiranjeevi
authors.forename: Uma
authors.initials: U
authors.lastname: Addepally
authors.forename: T S
authors.initials: TS
authors.lastname: Chinta Rao
authors.forename: Balaram
authors.initials: B
authors.lastname: Patro
mesh_terms: D000818:Animals; D001688:Biological Products / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D020552:Comet Assay; D006801:Humans; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy; D011161:Porifera / Q000737:chemistry; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001688:Biological Products; D011719:Pyrazines