Synthesis and antitumor activity of 20(S)-camptothecin derivatives: Carbamate-linked, water-soluble derivatives of 7-ethyl-10-hydroxycamptothecin

DOI: 10.1248/cpb.39.1446

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1446 - 1454 (1991)

Update date:2022-08-03

Topics:

Authors:

Sawada Sawada

Okajima Okajima

Aiyama Aiyama

Nokata Nokata

Furuta Furuta

Yokokura

Sugino Sugino

Yamaguchi

Miyasaka

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1248/cpb.39.1446

Novel 36 derivatives (6), bonding the phenolic hydroxyl group of 7-ethyl-10-hydroxycamptothecin (4) with diamines through a monocarbamate linkage, were synthesized and their antitumor activity was evaluated in vivo. The derivatives were soluble in water as their HCl salts with the E lactone ring intact and exhibited significant antitumor activity. One of the derivatives, 6-27 showed excellent activity against L1210 leukemia and other murine tumors. The structure of its hydrochloride trihydrate (CPT-11) was determined by spectroscopic and crystallographic methods.

Full text of DOI:10.1248/cpb.39.1446

NII-Electronic Library Service

Products guided by the article

Product name:4-Methyl-[1,4]diazepane-1-carboxylic acid (S)-4,11-diethyl-4-hydroxy-3,13-dioxo-3,4,12,13-tetrahydro-1H-2-oxa-6,12a-diaza-dibenzo[b,h]fluoren-9-yl ester

Cas No:136539-41-8

R&D Labs maybe for 136539-41-8

Shenyang Xinyihan Chemical Technology Co., Ltd.

Contact:+86-18525026267

Address:362, aigongbeijei street 23 , tiexi district,Shenyang, Liaoning, China
HANWAYS CHEMPHARM CO.,LIMITED

website:http://www.hanwayschem.com

Contact:+86-18502787239(whatsapp)-

Address:18-1-802, Green Garden, Jianghan District, Wuhan 430023, China
Suzhou Wedo Chemicals Co., Ltd.

Contact:86 512 58100425

Address:Zonger Road, DongSha Industry Park , Zhangjiagang, Jiangsu, China
Hebei DaPeng Pharm & Chem Co., Ltd.

Contact:86-317-7298678,0576-88861898 88861908

Address:West Songmen Village, East Songmen Town, Wuqiao, Cangzhou, Hebei ,China
CHEM PLUS

Contact:0027-717-456976

Address:2ND FLOOR, 325 VAUSE ROAD, OVERPORT, 4001, SOUTH AFRICA

Relevant to this article

Enantioselective approach to the synthesis of cyclohexane carbocyclic nucleosides

Doi:10.1021/jo972285c
(1998)
Doi:10.1007/BF02988706
(1881)
Metal complexes of ferrocenecarboxaldehyde 2,4-dichlorobenzoylhydrazone

Doi:10.1081/SIM-100002048
(2001)
Mechanism of selective formation of 2-amino-substituted 1,4-benzodiazepin-4-oxides and 2-aminomethyl substituted quinazolin-3-oxides from chloromethyl quinazolin-N-oxides indications from perturbation theory

Doi:10.1002/ardp.19943270204
(1994)
Regioselective catalytic allylic alkylation directed by removable 2-PyMe₂Si group

Doi:10.1021/ja0157346
(2001)
Doi:10.1080/10473289.2002.10470841
(1932)

Article Doi