title: Synthesis and cytotoxicity evaluation of (tetrahydro-beta-carboline)-1,3,5-triazine hybrids as anticancer agents.
abstract: A series of tetrahydro-beta-carbolines and 1,3,5-triazine hybrids have been synthesized and evaluated for their cytotoxicity against a panel of eight human cancer cell lines and normal human fibroblasts (NIH3T3). It led us to discovery of racemic compounds 69, 71 and 75, which are selectively cytotoxic towards KB (oral cancer) cell line with IC50 values of 105.8, 664.7 and 122.2 nM, respectively; while their enantiopure forms are less active and not selective. Enantiopure compound 42 showed 2.5 times more selectivity towards MCF7 cells over normal fibroblast NIH3T3 cells with an IC50 value of 740 nM, also arrests cell cycle in G1 phase and induces apoptosis in MCF7 and MDA MB231 cell lines.
authors.affiliation: Division of Medicinal & Process Chemistry, Central Drug Research Institute, CSIR, Lucknow 226001, India.
authors.forename: Ravi
authors.initials: R
authors.lastname: Kumar
authors.forename: Leena
authors.initials: L
authors.lastname: Gupta
authors.forename: Pooja
authors.initials: P
authors.lastname: Pal
authors.forename: Shahnawaz
authors.initials: S
authors.lastname: Khan
authors.forename: Neetu
authors.initials: N
authors.lastname: Singh
authors.forename: Sanjay Babu
authors.initials: SB
authors.lastname: Katiyar
authors.forename: Sanjeev
authors.initials: S
authors.lastname: Meena
authors.forename: Jayanta
authors.initials: J
authors.lastname: Sarkar
authors.forename: Sudhir
authors.initials: S
authors.lastname: Sinha
authors.forename: Jitendra Kumar
authors.initials: JK
authors.lastname: Kanaujiya
authors.forename: Savita
authors.initials: S
authors.lastname: Lochab
authors.forename: Arun Kumar
authors.initials: AK
authors.lastname: Trivedi
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002243:Carbolines / Q000737:chemistry*; D045744:Cell Line, Tumor; D053938:DNA Fragmentation / Q000187:drug effects; D016193:G1 Phase / Q000187:drug effects; D006801:Humans; D008938:Mitosis / Q000187:drug effects; D014227:Triazines / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines; D014227:Triazines