Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

M. Vijaya Bhaskar Reddy; Wei Jern Tsai; Keduo Qian; Kuo Hsiung Lee; Tian Shung Wu

doi:10.1016/j.bmc.2011.08.004

Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

M. Vijaya Bhaskar Reddy, Wei Jern Tsai, Keduo Qian, Kuo Hsiung Lee, Tian Shung Wu

School of Pharmacy

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

14 Citations (Scopus)

Abstract

In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL). In addition, the platelet aggregation activity of previously synthesized Mannich bases of heterocyclic chalcones (MBHC) (24-62) was evaluated. The preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3′ in ring-A of the MBHC templates.

Original language	English
Pages (from-to)	7711-7719
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	19
Issue number	24
DOIs	https://doi.org/10.1016/j.bmc.2011.08.004
Publication status	Published - 2011 Dec 15

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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title = "Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation",

abstract = "In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL). In addition, the platelet aggregation activity of previously synthesized Mannich bases of heterocyclic chalcones (MBHC) (24-62) was evaluated. The preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3′ in ring-A of the MBHC templates.",

author = "{Vijaya Bhaskar Reddy}, M. and Tsai, {Wei Jern} and Keduo Qian and Lee, {Kuo Hsiung} and Wu, {Tian Shung}",

note = "Funding Information: This work was supported by a Grant of National Science Council, Taiwan, Republic of China , and Grant No.( OUA 95-3-2-021 ) from the National Cheng Kung University, Tainan, Taiwan R.O.C awarded to T. S. Wu. This study is supported in part by Taiwan Department of Health Clinical Trial and Research Center of Excellence ( DOH100-TD-B-111-004 ).",

year = "2011",

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doi = "10.1016/j.bmc.2011.08.004",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

AU - Vijaya Bhaskar Reddy, M.

AU - Tsai, Wei Jern

AU - Qian, Keduo

AU - Lee, Kuo Hsiung

AU - Wu, Tian Shung

N1 - Funding Information: This work was supported by a Grant of National Science Council, Taiwan, Republic of China , and Grant No.( OUA 95-3-2-021 ) from the National Cheng Kung University, Tainan, Taiwan R.O.C awarded to T. S. Wu. This study is supported in part by Taiwan Department of Health Clinical Trial and Research Center of Excellence ( DOH100-TD-B-111-004 ).

PY - 2011/12/15

Y1 - 2011/12/15

N2 - In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL). In addition, the platelet aggregation activity of previously synthesized Mannich bases of heterocyclic chalcones (MBHC) (24-62) was evaluated. The preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3′ in ring-A of the MBHC templates.

AB - In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL). In addition, the platelet aggregation activity of previously synthesized Mannich bases of heterocyclic chalcones (MBHC) (24-62) was evaluated. The preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3′ in ring-A of the MBHC templates.

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