New Natural Products Under Development at the National Cancer Institute

Douros, John; Suffness, Matthew

doi:10.1007/978-3-642-81565-2_14

Cited by 33 publications

(9 citation statements)

References 25 publications

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“…On the other hand, phenanthroline, azaindolizine and phenanthridine derivatives were successful identified as DNA intercalating agents or possessing antimycobacterial activity 26,30,[40][41][42][43] . In the same time, benzo[c]phenanthridinium alkaloids as fagaronine and nitidine which showed antileukemic activity on rodents 44 and act as topoisomerase I and II inhibitors [45][46][47] , played the role of model compound for the development of new anticancer agents 14 . Having all these above consideration in mind and encouraged by our previous promising results in the field of anti-TB [25][26][27][28] and anticancer 29,30,32 derivatives with indolizine and/or phenanthroline skeleton, we have focused on the design of novel structures that contain four or five fused (hetero)cycles with pyrrolo[2,1-c] [4,7]phenanthroline skeleton (Scheme 3).…”

Section: Chemistrymentioning

confidence: 99%

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Matarneh

Mangalagiu

Shova³

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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A study concerning design, synthesis, structure and in vitro antimycobacterial and anticancer evaluation of new fused derivatives with pyrrolo[2,1-c] [4,7]phenanthroline skeleton is described. The strategy adopted for synthesis involves a [3 + 2] dipolar cycloaddition of several in situ generated 4,7-phenanthrolin-4-ium ylides to different substituted alkynes and alkenes. Stereo-and regiochemistry of cycloaddition reactions were discussed. The structure of the new compounds was proven unambiguously, single-crystal X-ray diffraction studies including. The antimycobacterial and anticancer activity of a selection of new synthesized compounds was evaluated against Mycobacterium tuberculosis H37Rv under aerobic conditions and 60 human tumour cell line panel, respectively. Five of the tested compounds possess a moderate antimycobacterial activity, while two of the compounds have a significant antitumor activity against renal cancer and breast cancer.

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Section: Chemistrymentioning

confidence: 99%

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Matarneh

Mangalagiu

Shova³

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…In the past, plant extracts were evaluated mainly in experimental animals, primarily mice and rats. The most extensive of these programs were sponsored by the National Cancer Institute (NCI) (24,(31)(32)(33)(34) (43,44).…”

Section: Approaches To Drug Discovery Using Higher Plantsmentioning

confidence: 99%

The Value of Plants Used in Traditional Medicine for Drug Discovery

Fabricant¹,

Farnsworth²

2001

Environmental Health Perspectives

624

674

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“…Effects of rapamycin (and rapalog)-induced mTOR inhibition on PA cellular proliferation and viability Rapamycin (sirolimus) is an immunosuppressant and antiproliferative agent that has previously been shown to be effective at abrogating cancer-related properties in a number of tumors (Douros & Suffness 1981, Majumder et al 2004. Specifically, rapamycin binds to the mTORC1 complex, affecting downstream signaling events including cell cycle arrest and protein synthesis inhibition.…”

Section: Current Mtor Inhibitorsmentioning

confidence: 99%

The PI3K/AKT/mTOR pathway in the pathophysiology and treatment of pituitary adenomas

Monsalves¹,

Juraschka²,

Tateno³

et al. 2014

Endocrine-Related Cancer

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Pituitary adenomas are common intracranial neoplasms. Patients with these tumors exhibit a wide range of clinically challenging problems, stemming either from results of sellar mass effect in pituitary macroadenoma or the diverse effects of aberrant hormone production by adenoma cells. While some patients are cured/controlled by surgical resection and/or medical therapy, a proportion of patients exhibit tumors that are refractory to current modalities. New therapeutic approaches are needed for these patients. Activation of the AKT/phophotidylinositide-3-kinase pathway, including mTOR activation, is common in human neoplasia, and a number of therapeutic approaches are being employed to neutralize activation of this pathway in human cancer. This review examines the role of this pathway in pituitary tumors with respect to tumor biology and its potential role as a therapeutic target.

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New Natural Products Under Development at the National Cancer Institute

Cited by 33 publications

References 25 publications

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

The Value of Plants Used in Traditional Medicine for Drug Discovery

The PI3K/AKT/mTOR pathway in the pathophysiology and treatment of pituitary adenomas

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