Delving into the Latest Updates on BE-14348B with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

BE14348B, WS 7528, WS-7528

Target

ER

Action

antagonists

Mechanism

ERs antagonists(Estrogen receptors antagonists)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Breast CancerNeoplasms

Originator Organization

Astellas Pharma, Inc.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.Fujisawa Pharmaceutical Co., Ltd.

Astellas Pharma, Inc.

License Organization-

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC16H14O5

InChIKeyGRHSSRUEUOYZIV-BCTVWOGZSA-N

CAS Registry132147-69-4

Streptomyces graminofaciens BA14348, isolated from a soil sample, was found to produce new specific inhibitors of estrogen binding to its receptor. Five related substances, BE-14348A approximately E, were isolated, and their structures were determined by analyses of spectral properties. Of these substances, A was identical with the known flavanone, naringenin. On the other hand, B, C, D and E were all new compounds; the structure of B was determined to be 2(S): 3(S)-3-methyl-4',5,7-trihydroxyflavanone, C was a racemic mixture of 2(S): 3 (R) and 2(R): 3(S)-3-methyl-4',5,7-trihydroxyflavanone; D and E were 8-chloro derivatives of B and C, respectively.

01 Jan 1990·The Journal of antibioticsQ4 · MEDICINE

WS-7528, a new isoflavanone with estrogen activity isolated from streptomyces sp. No. 7528. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.

Q4 · MEDICINE

Article

Author: Hashimoto, Masashi ; Uchida, Itsuo ; Tanaka, Miho ; Kiyoto, Sumio ; Kohsaka, Masanobu ; Yagi, Masashi ; Okuhara, Masakuni ; Nakayama, Osamu

WS-7528, produced by Streptomyces sp. No. 7528, was extracted from cultured broth, purified by solvent extraction followed by chromatography on silica gel and then isolated as pale yellow powder (C16H14O5, mp 95-98 degrees C). WS-7528 inhibited estrogen binding to its receptor protein in rat uterine cytosol. The IC50 value of WS-7528 for partially purified rat uterine cytosol receptor was 5.7 x 10(-8) M. This compound was found to induce the growth of the estrogen dependent cell line MCF-7. WS-7528 was tested orally and subcutaneously in immature rats to confirm its effect on the growth of the uterus. WS-7528 has also weak anti-inflammatory activity on the carrageenin paw edema of the rat model.

100 Deals associated with BE-14348B

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Preclinical	-	Astellas Pharma, Inc.	-
Breast Cancer	Preclinical	-	Merck Sharp & Dohme Corp.	-
Neoplasms	Preclinical	Japan	Fujisawa Pharmaceutical Co., Ltd.	-