2. Academic Validation
  3. Synthesis of novel benzylidene analogues of betulinic acid as potent cytotoxic agents

Synthesis of novel benzylidene analogues of betulinic acid as potent cytotoxic agents

  • Eur J Med Chem. 2017 Jul 28:135:517-530. doi: 10.1016/j.ejmech.2017.04.062.
Nidhi Gupta 1,  Santosh K Rath 2,  Jasvinder Singh 3,  Arem Qayum 3,  Shashank Singh 4,  Payare L Sangwan 5
Affiliations

Affiliations

  • 1 Bioorganic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India.
  • 2 Bioorganic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM Campus, Jammu, India.
  • 3 Cancer Pharmacology Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM Campus, Jammu, India.
  • 4 Cancer Pharmacology Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM Campus, Jammu, India. Electronic address: sksingh@iiim.ac.in.
  • 5 Bioorganic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM Campus, Jammu, India. Electronic address: plsangwan@iiim.ac.in.
PMID: 28500966 DOI: 10.1016/j.ejmech.2017.04.062
Abstract

Different benzylidene derivatives (15a-o and 16a-o) of betulinic acid were designed and synthesized in an effort to develop potent Anticancer agents. All the synthesized derivatives along with betulinic acid were evaluated for cytotoxicity against a panel of five different human Cancer cell lines A-549 (Lung), PC-3 (Prostate), HCT 116 (Colon), MCF-7 (Breast) and MIA PaCa-2 (Pancreatic) using SRB assay. Pharmacological results showed that compounds 15b, 15c, 15i, 15k, 16a-c and 16l were found to have promising cytotoxic profile against various Cancer cell lines tested (IC50 1-2 μM). Best results were observed for compound 16c with IC50 values 1.5, 1.6, 1.36, 3.5 and 3.2 μM against A-549, PC-3, HCT 116, MCF-7 and MIA PaCa-2 cell lines, respectively. Mechanistic study of compound 16c revealed that it inhibits the colony formation and restrict the migration in HCT 116 cells in vitro. It also induces growth arrest with characterized morphological changes and loss of mitochondrial membrane potential (MMP) in a concentration dependent manner.

Keywords

Benzylidene derivatives; Betulinic acid; Colony formation; Cytotoxicity.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z