Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0025202 (melanoma)
 69,561 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Thirty-one aziridinylbenzoquinones were compared against five murine tumor models in vivo. Two intracerebral (ependymoblastoma and L-1210 leukemia) and three intraperitoneal (P-388 and L-1210 leukemia and B16 melanoma) systems were utilized. Excellent activity was observed for many compounds. Multiple long-term survivors were produced in the ependymoblastoma, P-388, and intraperitoneal L-1210 systems. Diethyl 2,5-bis(1-aziridinyl)-3,6-dioxo-1,4-cyclohexadiene-1,4-dicarbamate demonstrated superior activity in all five test systems. This compound also was reproducibly active against two colon tumors, a mammary tumor, and the intracerebrally implanted P-388 leukemia model.
 ...
PMID:Potential CNS antitumor agents VI: aziridinylbenzoquinones III. 42 89

1,4-Dihydroxy-5,8-bis(((2[(2-hydroxyethyl)amino]ethyl)amino))-9,-10-anthracenedione dihydrochloride (CL 232315; NSC 301739D), a representative of a new chemical class of compounds with antineoplastic properties, has been evaluated for antitumor activity in experimental mouse tumor systems. The compound produced significant increases in life span (ILS) and long-term survivors when tested against the P388 and L1210 leukemias as well as the solid neoplasms, B16 melanoma and Colon Tumor 26. The optimal treatment regimens resulted in a 173 to greater than 200% ILS with 20 to 80% 60-day survivors in mice with P388 leukemia, A 205% ILS with 55% 60-day survivors in mice with L1210 leukemia, and an ILS of greater than 300% with 80% 90-day survivors in mice with B16 melanoma. In contrast to Adriamycin, CL 232315 was active against the i.v. implanted L1210 leukemia and demonstrated moderate activity against P388/Adria, a subline of P388 resistant to Adriamycin. The compound was ineffective when tested against the Lewis lung carcinoma and the Ridgway osteogenic sarcoma. CL 232315 was active i.p., s.c., and i.v., but p.o. activity was not demonstrated. Schedule dependency was not observed when the compound was administered once daily for nine days, once every four days, or as a single dose.
 ...
PMID:Activity of a novel anthracenedione, 1,4-dihydroxy-5,8-bis(((2-[(2-hydroxyethyl)amino]ethyl)amino])-9,10-anthracenedione dihydrochloride, against experimental tumors in mice. 42 98

While structure-activity relationships for vinblastine (VLB), vincristine, deacetyl-VLB, and deacetyl-VLB amide (vindesine, VDS) in several tumor and leukemia models have been reported previously, the present study explores these relationships for a series of N-substituted vindesine analogues. These compounds were prepared from the reaction of deacetyl-VLB acid azide with the appropriate amines and were characterized by mass spectral analysis, 1H and 13C NMR spectra, electrometric titration, and infrared spectra. N-Alkylvindesines have reduced activity compared to that of VDS against the Gardner lymphosarcoma (GLS). N-beta-Hydroxyethyl-VDS surpasses vindesine in its activity against the Ridgway osteogenic sarcoma and the GLS, whereas against the B16 melanoma it is less active than VDS. N-beta-(4-Hydroxyphenethyl)-VDS, envisaged as a substrate for the enzyme tryosinase, was shown to be more active than VDS against the B16 melanoma but has only marginal activity against the GLS. In terms of collective antitumor activity against the model systems used, vindesine emerges as the congener with optimum qualities. Bis(N-ethylidenevindesine) disulfide, the first example of a bridged bisvindesine and comparable to VDS in its antitumor profile, shows evidence of activity against a P388/VCR leukemia strain known to be resistant to maytansine as well as to vincristine.
 ...
PMID:Structure-activity relationships of dimeric Catharanthus alkaloids. 2. Experimental antitumor activities of N-substituted deacetylvinblastine amide (vindesine) sulfates. 43 Apr 77

Total protein and sialic acid levels were determined in the supernatant of serum treated with perchloric acid. Patients with either localized or advanced metastatic malignancy have significantly elevated mean serum values. The highest levels occur in patients with lung, GI, GYN cancer, lymphoma and malignant melanoma. Patients with leukemia and multiple myeloma have slightly elevated values, but they were not significantly different from normal. Patients following curative surgery have normal values while patients in clinical remission following chemotherapy have elevated mean serum protein and NANA levels. Elevated values also occur in patients with benign tumors and 12% of patients with nonmalignant disease. Tumor cells appear to shed macromolecules which contribute to the observed elevation of serum protein and sialic acid levels.
 ...
PMID:Glycoproteins and human cancer. 1. Circulating levels in cancer serum. 44 66

A novel nitrosourea derivative, methyl-6-[[[(2-chloroethyl)nitrosoamino]carbonyl]-amino]-6-deoxy-alpha-D-glucopyranoside (MCNU), is a water-soluble compound in which a methoxyl group is attached to the C-1 position and an N-(2-chloroethyl)-N-nitrosoureido group is attached to the C-6 position of the glucose moiety. MCNU exhibited a marked life-prolongation or growth-inhibitory effect against mouse L1210 leukemia, adenocarcinoma 755, Nakahara-Fukuoka sarcoma, Lewis lung carcinoma, and B16 melanoma. Ip, oral, or iv administration of MCNU was markedly effective against L1210 leukemia, and the therapeutic ratio by ip administration was larger than that of chlorozotocin or CCNU. The life-prolongation effect of MCNU against established Lewis lung carcinoma was similar to that of methyl-CCNU. The bone marrow toxicity of MCNU was less than that of CCNU but considerably more than that of chlorozotocin.
 ...
PMID:Biologic activity of MCNU: a new antitumor agent. 46 55

The cause-specific mortality experience of 826 plant employees and 249 sales representatives employed by a large U.S. pharmaceutical firm was examined to determine if there were unusual patterns of fatal disease that might relate to factors in the work environment. Deaths that occurred between 1954 and 1976 among actively employed or retired workers were identified through company records and a proportionate mortality analysis was carried out using the total U.S. as a standard. PMRs were computed for male and for female workers and for several broad occupational categories. A significant difference between observed and expected mortality from suicide was present in both males and females and there was an indication that drug overdoses were over-represented. PMRs for several cancer sites were elevated, but excesses were not always confined to particular occupational categories. Excesses of respiratory cancer were present in male maintenance workers and in female production workers. Increased relative frequencies of melanoma among males and of leukemia among females were confined to the production worker category. Some of the findings may provide leads for further investigations of the pharmaceutical industry.
 ...
PMID:Mortality among workers employed in the pharmaceutical industry: a preliminary investigation. 49 Feb 23

The condensation of alkylenediamines with quinizarin or with 2,3-dihydro-1,4,5,8-tetrahydroxy-9,10-anthracenedione, followed by oxidation, gave 1,4-bis[aminoalkyl)amino]-9,10-anthracenediones. Some of these compounds and their 2,3-dihydro derivatives were markedly active against both leukemias and solid tumors in mice. Activity was maximal with 5,8-dihydroxylation and 1,4-bis[(2-aminoethyl)amino] substitution, in which the terminal nitrogen atoms were either unsubstituted (compound 50) or carried 2-hydroxyethyl groups (compound 40), indicating the importance of hydrophilicity. Against B-16 melanoma, 50 gave greater than 433% increase in median life span (ILS) with 7/10 80-day survivors. Against P-388 leukemia, 40 gave greater than 500% ILS with 4/5.60-day survivors; its efficacy and therapeutic index equaled or surpassed those of adriamycin, cyclophosphamide, daunorubicin, methotrexate, or 5-fluorouracil. Against L-1210 leukemia, B-16 melanoma, and colon tumor 26, 40 was generally as effective or more effective than adriamycin and is now undergoing preclinical toxicological evaluation.
 ...
PMID:Antitumor agents. 1. 1,4-Bis[(aminoalkyl)amino]-9,10-anthracenediones. 49 May 45

cis-Dichlorodiammineplatinum(II) has shown good broad-spectrum activity in the current Division of Cancer Treatment (National Cancer Institute) tumor panel. It meets Decision Network criteria for activity in at least five of ten tumor systems (the ip B16 melanoma, the sc CD8F1 mammary carcinoma, the ip colon tumor 26, the ip L1210 leukemia, and the ip P388 leukemia). Activity against the sc colon tumor 38, the iv Lewis lung tumor, the ic ependymoblastoma, and the human breast tumor xenograft (MX-1) was marginal. No activity was detected against the human lung tumor xenograft (LX-1), but good, reproducible activity was observed against the murine M5076 ovarian carcinoma. No schedule-dependency was observed after ip administration against the ip L1210 leukemia. The recently developed subrenal capsule assay offers promise as a rapid way (less than or equal to 11 days) of ranking the sensitivity of a variety of human tumors to cis-dichlorodiammineplatinum(II) and other chemotherapeutic agents.
 ...
PMID:Antitumor activity of cis-dichlorodiammineplatinum(II). 49 46

A set of 23 aniline mustards [X-C6H4N(CH2CH2Cl)2] have been tested for their activity against B-16 melanoma in mice. The following quantitative structure-activity relationship (QSAR) correlates the data well: log 1/C = -2.06 sigma - 0.15 pi - 0.13 pi2 + 4.13 (r = 0.936). When this equation is compared with those formulated for aniline mustards acting against leukemia, it is found that log P0 (ideal lipophilicity) is higher for solid tumors. The QSAR brings out the unique activity of phenylalanine aniline mustard.
 ...
PMID:Structure-activity relationship of aniline mustards acting against B-16 melanoma in mice. 51 75

The bacterial flora of the skin from different anatomical sites on cancer patients and a control group of medical personnel was examined. This was done to ascertain if antineoplastic therapy was able to change the pattern of microbial flora of patients and to provide a control for possible infectious complications. The results show that in the control group bacterial flora was normal and the antineoplastic treatment did not succeed in changing the bacterial pattern in the skin of patients deeply. Gram negative bacteria were isolated more frequently from the skin of leukemia patients than from either patients with malignant melanoma or other neoplastic diseases.
 ...
PMID:[Changes in the bacterial flora of patients under antineoplastic treatment]. 51 58


<< Previous 1 2 3 4 5 6 7 8 9 10 Next >>