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acronycine/cáncer

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Marked antitumor activity of a new potent acronycine derivative in orthotopic models of human solid tumors.

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S 23906-1 is a novel acronycine derivative selected on the basis of its potency in vitro. We investigated the antitumor activity of S 23906-1 against several murine transplantable tumors (C38 colon carcinoma, P388 leukemia, B16 melanoma, and Lewis lung carcinoma) and in orthotopic models of human

Drug sensitivity testing of carcinoma of the gallbladder and biliary tree in a human tumor cloning assay.

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We have received and attempted to culture 27 specimens from 26 patients with carcinoma of the gallbladder and biliary tree. Evaluable growth, defined as greater than or equal to 20 tumor colonies per control plate, was obtained in 8 (30%) of the specimens. Thirteen of the specimens (48%) did not

Synthesis and cytotoxic and antitumor activity of 1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diacid hemiesters and carbamates.

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A series of cis-1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diacid hemiesters and dicarbamates were prepared by acylation of cis-1,2-dihydroxy-6-methoxy-3,3,14-trimethyl-1,2,3,14-tetrahydro-7H-benzo[b]pyrano[3,2-h]acridin-7-one. The cytotoxicity of the dicarbamates depended on the steric hindrance

Synthesis, antitumor activity, and mechanism of action of benzo[b]chromeno[6,5-g][1,8]naphthyridin-7-one analogs of acronycine.

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A series of 6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]chromeno[6,5-g][1,8]naphthyridin-7-one (4), 13-aza derivatives of benzo[b]acronycine, the isomeric 5-methoxy-2,2,13-trimethyl-2,13-dihydro-6H-benzo[b]chromeno[7,6-g][1,8]naphthyridin-6-one (5), and related cis-diols mono- and diesters
S23906-1 is a benzo[b]acronycine derivative acting as a DNA-alkylating agent through covalent bonding to the exocyclic amino group of guanines and subsequent local opening of the DNA helix. This compound was selected for phase I clinical trials based on its efficient antitumor activity in
Acronycine (I) is a broad-spectrum antitumor agent whose development as a clinically useful agent has been hindered, in part, due to its poor solubility characteristics. With the goal of acquiring information that may prove of value in the development of structurally related compounds of greater

[Structure activity relationships and mechanism of action of antitumor benzo[b]acronycine antitumor agents].

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The acridone alkaloid acronycine, isolated from several Sarcomelicope species (Rutaceae) was shown to exhibit a promising activity against a broad spectrum of solid tumors. Nevertheless, subsequent clinical trials only gave poor results, probably due to the moderate potency of this drug. The

A transesterification reaction is implicated in the covalent binding of benzo[b]acronycine anticancer agents with DNA and glutathion.

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The benzo[b]acronycine derivative S23906-1 has been recently identified as a promising antitumor agent, showing remarkable in vivo activities against a panel of solid tumors. The anticancer activity is attributed to the capacity of the drug to alkylate DNA, selectively at the exocyclic 2-amino group

Antitumor activity and murine pharmacokinetics of parenteral acronycine.

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The lipophilic antitumor alkaloid acronycine (ACRO) was solubilized in the cosolvent system used for etoposide. ACRO in this etoposide diluent (VPD) was found to be cytotoxic (less than or equal to 50% colony formation in soft agar) in fresh human tumors from patients with renal cell cancer, ovarian

[New antitumor agents in the acronycine series].

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The acridone alkaloid acronycine, isolated from several Sarcomelicope species (Rutaceae) was shown to exhibit a promising activity against a broad spectrum of solid tumors. Nevertheless, clinical trials only gave poor results, probably due to the moderate potency of this drug. The isolation of the

[Acronycine revisited: development of benzo[b]acronycine antitumor agents].

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The acridone alkaloid acronycine, isolated from several Sarcomelicopespecies (Rutaceae) was shown to exhibit a promising activity against a broad spectrum of solid tumors. Nevertheless, subsequent clinical trials gave limited results, probably due to the moderate potency and poor water solubility of

Acronycine derivatives as promising antitumor agents.

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Originally isolated from an Australian plant, acronycine is an antitumor alkaloid with poor water solubility and low potency. The modest antitumor activity of this compound was markedly improved by the total synthesis of original analogs resulting in the selection of S23906-1, a diester derivative

Bioassay of acronycine for possible carcinogenicity.

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A bioassay of acronycine for possible carcinogenicity was conducted by administering the test chemical by intraperitoneal injection to Sprague-Dawley rats and B6C3F1 mice. Initially, groups of 35 rats of each sex were administered acronycine at one of two doses, either 7.5 or 15 mg/kg body weight,

[From acronycine to benzo-[b]-acronycine derivatives: potent antitumor agents].

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The acridone alkaloid acronycine, first isolated in 1948, was shown in 1966 to have promising activity against a range of solid tumors. Clinical trials conducted in 1983 gave disappointing results, however, probably owing to the moderate potency of this drug. Our isolation of the unstable molecule

Synthesis and cytotoxic and antitumor activity of benzo[b]pyrano[3, 2-h]acridin-7-one analogues of acronycine.

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Benzo¿băcronycine (6-methoxy-3,3,14-trimethyl-3, 14-dihydro-7H-benzo¿bpyrano¿3,2-hăcridin-7-one, 4), an acronycine analogue with an additional aromatic ring linearly fused on the natural alkaloid basic skeleton, was synthesized in three steps, starting from 3-amino-2-naphthalenecarboxylic acid (5).
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