Synthesis of novel β-carboline based chalcones with high cytotoxic activity against breast cancer cells.
A series of novel β-carboline based chalcones was synthesized and evaluated for their cytotoxic activity against a panel of human cancer cell lines. Among them we found that two of the compounds 7c and 7d, showed marked anti-proliferative activity in a panel of solid tumor cell lines with highest effect in breast cancer. The compounds 7c and 7d showed an IC50 of 2.25 and 3.29 μM, respectively against human breast cancer MCF-7 cell line. Further, the compound 7c markedly induced DNA fragmentation and apoptosis in breast cancer cells.
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India; Department of Chemistry, Integral University, Lucknow 226 026, U.P., India.
Shikha S
SS
Chauhan
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Anup K
AK
Singh
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Sanjeev
S
Meena
Department of Chemistry, Integral University, Lucknow 226 026, U.P., India.
Minaxi
M
Lohani
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Akhilesh
A
Singh
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Rakesh K
RK
Arya
Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Srikanth H
SH
Cheruvu
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Jayanta
J
Sarkar
Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Jiaur R
JR
Gayen
Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Dipak
D
Datta
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India. Electronic address: prem_chauhan_2000@yahoo.com.
Prem M S
PM
Chauhan
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002243:Carbolines / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D053938:DNA Fragmentation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000970:Antineoplastic Agents; D002243:Carbolines; D047188:Chalcones
Anticancer; Chalcone; Cytotoxic; β-Carboline