Betulinic Acid Derivatives as Anticancer Agents: Structure Activity Relationship

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Betulinic Acid Derivatives as Anticancer Agents: Structure Activity Relationship

Anti-Cancer Agents in Medicinal Chemistry, 6(3): 271-279.

Author(s): Rama Mukherjee, Vivek Kumar, Sanjay K. Srivastava, Shiv K. Agarwal and Anand C Burman.

Affiliation: Medicinal Chemistry, DaburResearch Foundation, 22, Site IV, Sahibabad, Ghaziabad 201010, UP, India.


Betulinic acid, a pentacyclic triterpene, is widely distributed throughout the tropics. It possesses several biological properties such as anticancer, anti-inflammatory, antiviral, antiseptic, antimalarial, spermicidal, antimicrobial, antileshmanial, antihelmentic and antifeedent activities. However, betulinic acid was highly regarded for its anticancer and anti-HIV activities. Anticancer role of betulinic acid appeared by inducing apoptosis in cells irrespective of their p53 status. Due to high order safety in betulinic acid, a number of structural modifications carried out to improve its potency and efficacy. The C-1, C-2, C-3, C-4, C-20 and C-28 positions are the diversity centers in betulinic acid, and the derivatives resulted on various structural modifications at these positions screened for their anticancer activity. This review presents the structure activity relationship carried out on C-1, C-2, C-3, C-4, C-20, C-28, A-ring, D-ring and E-ring modified betulinic acid derivatives. We have compiled the most active betulinic acid derivatives along with their activity profile in each series. Structure activity relationship studies revealed that C-28 carboxylic acid was essential for the cytotoxicity. The halo substituent at C-2 position in betulinic acid enhanced the cytotoxicity. Though the relation of the cytotoxicity with the nature of substituents at C-3 position could not be generalized but the ester functionality appeared to be a better substituent for enhancing the cytotoxicity. An interesting observation is that the three rings skeleton (A, B and C rings) had played an important role in eliciting anticancer activity, which could be a new molecular skeleton to design new anticancer drugs.


Betulinic acid, Betulinic acid derivatives, Anticancer, Structure activity relationship (SAR).

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Article Details

Volume: 6
Issue Number: 3
First Page: 271
Last Page: 279
Page Count: 9
DOI: 10.2174/187152006776930846
Price: $58

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