Bakuchiol derivatives as novel and potent cytotoxic agents: A report

Rabiya Majeed; Mallepally V. Reddy; Praveen K. Chinthakindi; Payare L. Sangwan; Abid Hamid; Gousia Chashoo; Ajit K. Saxena; Surrinder Koul

doi:10.1016/j.ejmech.2011.12.018

Bakuchiol derivatives as novel and potent cytotoxic agents: A report

Rabiya Majeed, Mallepally V. Reddy, Praveen K. Chinthakindi, Payare L. Sangwan, Abid Hamid, Gousia Chashoo, Ajit K. Saxena, Surrinder Koul

Research output: Contribution to journal › Article › peer-review

43 Scopus citations

Abstract

A library of 28 compounds comprising of acyl, amino, halo, nitro, styryl and cyclized derivatives of bakuchiol have been evaluated against a panel of eight human cancer cell lines. Bioevaluation studies have resulted in the identification of potent cytotoxic molecules exhibiting concentration dependent growth inhibition against leukemia cancer cells with best results observed for compounds 17 and 22 exhibiting IC ₅₀ 1.8 and 2.0 μM respectively. As evident from various biological end-points, inhibition of cell proliferation by inducing G2/M cell cycle arrest, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis is demonstrated.

Original language	English
Pages (from-to)	55-67
Number of pages	13
Journal	European Journal of Medicinal Chemistry
Volume	49
DOIs	https://doi.org/10.1016/j.ejmech.2011.12.018
State	Published - Mar 2012
Externally published	Yes

Keywords

Apoptosis
Bakuchiol analogs
Cell cycle analysis
Heck coupling
Mercuration-demercuration

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10.1016/j.ejmech.2011.12.018

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title = "Bakuchiol derivatives as novel and potent cytotoxic agents: A report",

abstract = "A library of 28 compounds comprising of acyl, amino, halo, nitro, styryl and cyclized derivatives of bakuchiol have been evaluated against a panel of eight human cancer cell lines. Bioevaluation studies have resulted in the identification of potent cytotoxic molecules exhibiting concentration dependent growth inhibition against leukemia cancer cells with best results observed for compounds 17 and 22 exhibiting IC 50 1.8 and 2.0 μM respectively. As evident from various biological end-points, inhibition of cell proliferation by inducing G2/M cell cycle arrest, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis is demonstrated.",

keywords = "Apoptosis, Bakuchiol analogs, Cell cycle analysis, Heck coupling, Mercuration-demercuration",

author = "Rabiya Majeed and Reddy, {Mallepally V.} and Chinthakindi, {Praveen K.} and Sangwan, {Payare L.} and Abid Hamid and Gousia Chashoo and Saxena, {Ajit K.} and Surrinder Koul",

note = "Funding Information: The authors are thankful to Dr. SN Sharma (Taxonomist, IIIM, Jammu) for providing the authentic plant material. Authors (MVR and PKC) gratefully thank Council of Scientific and Industrial Research (CSIR), New Delhi for the award of senior research fellowships. Director IIIM is well acknowledged for encouragement of the work. ",

year = "2012",

month = mar,

doi = "10.1016/j.ejmech.2011.12.018",

language = "English",

volume = "49",

pages = "55--67",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

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T1 - Bakuchiol derivatives as novel and potent cytotoxic agents

T2 - A report

AU - Majeed, Rabiya

AU - Reddy, Mallepally V.

AU - Chinthakindi, Praveen K.

AU - Sangwan, Payare L.

AU - Hamid, Abid

AU - Chashoo, Gousia

AU - Saxena, Ajit K.

AU - Koul, Surrinder

N1 - Funding Information: The authors are thankful to Dr. SN Sharma (Taxonomist, IIIM, Jammu) for providing the authentic plant material. Authors (MVR and PKC) gratefully thank Council of Scientific and Industrial Research (CSIR), New Delhi for the award of senior research fellowships. Director IIIM is well acknowledged for encouragement of the work.

PY - 2012/3

Y1 - 2012/3

N2 - A library of 28 compounds comprising of acyl, amino, halo, nitro, styryl and cyclized derivatives of bakuchiol have been evaluated against a panel of eight human cancer cell lines. Bioevaluation studies have resulted in the identification of potent cytotoxic molecules exhibiting concentration dependent growth inhibition against leukemia cancer cells with best results observed for compounds 17 and 22 exhibiting IC 50 1.8 and 2.0 μM respectively. As evident from various biological end-points, inhibition of cell proliferation by inducing G2/M cell cycle arrest, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis is demonstrated.

AB - A library of 28 compounds comprising of acyl, amino, halo, nitro, styryl and cyclized derivatives of bakuchiol have been evaluated against a panel of eight human cancer cell lines. Bioevaluation studies have resulted in the identification of potent cytotoxic molecules exhibiting concentration dependent growth inhibition against leukemia cancer cells with best results observed for compounds 17 and 22 exhibiting IC 50 1.8 and 2.0 μM respectively. As evident from various biological end-points, inhibition of cell proliferation by inducing G2/M cell cycle arrest, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis is demonstrated.

KW - Apoptosis

KW - Bakuchiol analogs

KW - Cell cycle analysis

KW - Heck coupling

KW - Mercuration-demercuration

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DO - 10.1016/j.ejmech.2011.12.018

M3 - Article

C2 - 22245048

AN - SCOPUS:84857239458

SN - 0223-5234

VL - 49

SP - 55

EP - 67

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Bakuchiol derivatives as novel and potent cytotoxic agents: A report

Abstract

Keywords

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