@entity69923 is a novel @entity54792 derivative selected on the basis of its potency in vitro. We investigated the antitumor activity of @entity69923 against several @entity19 transplantable @entity5 (C38 @entity694 , @entity23198 , @entity6844 , and @entity2 ) and in orthotopic models of @entity1 lung (NCI-H460 and A549), ovarian (IGROV1 and NIH:OVCAR-3), and @entity14 (HCT116 and HT-29). Against established C38 @entity694 , @entity69923 administered twice i.v. from 1.56-6.25 mg/kg markedly inhibited @entity5 growth. Treatment at the optimal dose (6.25 mg/kg) induced @entity5 regression in all of the @entity19 . @entity54792 was 16-fold less potent and only moderately active at the maximum tolerated dose, 100 mg/kg. Against other @entity19 @entity5 of the former National @entity5 Institute panel, @entity69923 was either only moderately active or totally inactive. When evaluated in @entity1 orthotopic models, @entity69923 given p.o. or i.v. demonstrated a marked antitumor activity against @entity1 @entity189 . In the two @entity1 @entity2 models, @entity69923 increased the survival of the animals in a dose-dependent manner and induced treated versus control values of 162% (NCI-H460) and 193% (A549). @entity1206 was less active, with treated versus control values of 119% and 174%, respectively. A significant survival benefit was also observed against the two i.p. @entity43 in which @entity69923 was as active as @entity1311 , inducing 80% long-term survivors in the NIH:OVCAR-3 model. Lastly, @entity69923 inhibited the growth of primary @entity694 grafted onto the cecum as efficiently as @entity2600 and eradicated the formation of lymph node, hepatic, and pulmonary metastases in the aggressive HCT116 model. The novel spectrum of activity of @entity69923 compared with existing anticancer agents warrants further preclinical investigation.

Marked antitumor activity of a new potent @entity54792 derivative in orthotopic models of XXXX @entity5 .

@entity1 :: ('9606', 'Species') :: ['human'] @entity43 :: ('MESH:D010051', 'Disease') :: ['ovarian tumors'] @entity23198 :: ('MESH:D007941', 'Disease') :: ['P388 leukemia'] @entity2600 :: ('MESH:C051890', 'Chemical') :: ['irinotecan'] @entity19 :: ('10090', 'Species') :: ['mice', 'murine'] @entity69923 :: ('MESH:C436732', 'Chemical') :: ['S 23906-1'] @entity5 :: ('MESH:D009369', 'Disease') :: ['tumor', 'Cancer', 'tumors'] @entity2 :: ('MESH:D008175', 'Disease') :: ['Lewis lung carcinoma', 'lung cancer'] @entity1311 :: ('MESH:D017239', 'Chemical') :: ['paclitaxel'] @entity189 :: ('MESH:D002277', 'Disease') :: ['carcinomas'] @entity1206 :: ('MESH:C030852', 'Chemical') :: ['Vinorelbine'] @entity6844 :: ('MESH:D008546', 'Disease') :: ['B16 melanoma'] @entity14 :: ('MESH:D015179', 'Disease') :: ['colorectal cancers'] @entity694 :: ('MESH:D003110', 'Disease') :: ['HT-29 and HCT116 colon tumors', 'colon carcinoma'] @entity54792 :: ('MESH:D000175', 'Chemical') :: ['Acronycine', 'acronycine']
@entity1 :: (9606,Species) :: ['human']
