Bizelesin

Names

[ Name ]:
Bizelesin

[Synonym ]:
Benzo(1,2-b:4,3-b')dipyrrol-4-ol,6,6'-(carbonylbis(imino-1H-indole-5,2-diylcarbonyl))bis(8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-,(S-(R*,R*))
U-77,779
BIZELESIN
Bizelesin (USAN/INN)

Biological Activity

[Description]:

Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker

[In Vitro]

Bizelesin (0-5 μM, 4 h)可以通过靶向人类癌细胞 CEM 细胞中富含 AT的 DNA 域，造成 DNA 特异性损伤，进而造成癌细胞损伤，具有潜在的癌症治疗潜力[1]。 Bizelesin (0-500 nM)在 BSC-1 细胞中，当浓度为 10 nM 时导致 50% 的 DNA 合成抑制，相比之下，浓度为 160 nM 时才抑制 50% RNA 合成，而浓度高达至 200 nM 时也没有观察到蛋白质合成的抑制[2]。

[References]

[1]. J M Woynarowski, et al. AT-rich islands in genomic DNA as a novel target for AT-specific DNA-reactive antitumor drugs. J Biol Chem. 2001 Nov 2;276(44):40555-66.

[2]. J M Woynarowski, et al. Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on replication of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta. 1997 Jul 17;1353(1):50-60.

Chemical & Physical Properties

[ Density]:
1.604g/cm3

[ Molecular Formula ]:
C₄₃H₃₆Cl₂N₈O₅

[ Molecular Weight ]:
815.70300

[ Exact Mass ]:
814.21900

[ PSA ]:
185.37000

[ LogP ]:
9.52540

[ Index of Refraction ]:
1.856

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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