Structure–activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

Hirokazu Tamamura; Ai Esaka; Teppei Ogawa; Takanobu Araki; Satoshi Ueda; Zixuan Wang; John O. Trent; Hiroshi Tsutsumi; Hiroyuki Masuno; Hideki Nakashima; Naoki Yamamoto; Stephen C. Peiper; Akira Otaka; Nobutaka Fujii

doi:10.1039/B513145F

Structure–activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds†

Hirokazu Tamamura,*^ab Ai Esaka,^b Teppei Ogawa,^b Takanobu Araki,^b Satoshi Ueda,^b Zixuan Wang,^c John O. Trent,^d Hiroshi Tsutsumi,^a Hiroyuki Masuno,^a Hideki Nakashima,^e Naoki Yamamoto,^f Stephen C. Peiper,^c Akira Otaka^bg and Nobutaka Fujii*^b

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^a Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo, Japan
E-mail: tamamura.mr@tmd.ac.jp
Fax: +81 3 5280 8039
Tel: +81 3 5280 8036

^b Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto, Japan
E-mail: nfujii@pharm.kyoto-u.ac.jp
Fax: +81 75 753 4570
Tel: +81 75 753 4551

^c Medical College of Georgia, Augusta, GA, USA

^d James Graham Brown Cancer Center, University of Louisville, Louisville, KY, USA

^e St. Marianna University, School of Medicine, Miyamae-ku, Kawasaki, Japan

^f AIDS Research Center, National Institute of Infectious Diseases, Shinjuku-ku, Tokyo, Japan

^g Graduate School of Pharmaceutical Sciences, The University of Tokushima, Tokushima, Japan

Abstract

Structure–activity relationship studies on CXCR4 antagonists, which were previously found by using cyclic pentapeptide libraries, were performed to optimize side-chain functional groups, involving conformationally constrained analogues. In addition, a new lead of cyclic pentapeptides with the introduction of a novel pharmacophore was developed.

Organic & Biomolecular Chemistry

Structure–activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds†

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Structure–activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

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