118930-99-7Relevant academic research and scientific papers
DUPA Conjugation of a Cytotoxic Indenoisoquinoline Topoisomerase i Inhibitor for Selective Prostate Cancer Cell Targeting
Roy, Jyoti,Nguyen, Trung Xuan,Kanduluru, Ananda Kumar,Venkatesh, Chelvam,Lv, Wei,Reddy, P. V. Narasimha,Low, Philip S.,Cushman, Mark
, p. 3094 - 3103 (2015/04/27)
(Figure Presented). Prostate-specific membrane antigen (PSMA) is overexpressed in most prostate cancer cells while being present at low or undetectable levels in normal cells. This difference provides an opportunity to selectively deliver cytotoxic drugs
DUPA-INDENOISOQUINOLINE CONJUGATES
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Paragraph 00213, (2015/05/26)
A targeting ligand-cytotoxic drug conjugate, for example, a DUPA-Indenoisoquinoline conjugate, is useful for treating cancers, e.g., prostate cancer.
CONJUGATES AND COMPOSITIONS FOR DRUG DELIVERY
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Paragraph 120, (2015/08/03)
The present invention provides folate receptor binding ligand‐drug delivery conjugates having the formula (F) nL1L2D. The conjugates have high affinity to folate receptor‐positive tumor cells and low toxicity for normal ce
PROCESSES FOR MAKING EPOTHILONE COMPOUNDS AND ANALOGS
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Page/Page column 49-50, (2009/01/20)
The present invention relates to processes for making epothilone compounds and analogs thereof, such as epi-epothilone A or epi-epothilone B, and aziridinyl-epothilone analogs.
Design and synthesis of releasable folate-drug conjugates using a novel heterobifunctional disulfide-containing linker
Satyam, Apparao
supporting information; experimental part, p. 3196 - 3199 (2009/04/11)
Cellular uptake of vitamin folic acid occurs via folate-receptor mediated endocytosis. Many types of cancer cells express high levels of folate receptors as they need continuous supply of this vitamin for their proliferation. With an objective to use foli
CONJUGATES OF AZIRIDINYL-EPOTHILONE ANALOGS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
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Page/Page column 27, (2008/06/13)
The present invention is directed to conjugated compounds comprising a folate, or an analog or derivative thereof, and an aziridinyl epothilone analog, as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof, useful i
AZIRIDINYL-EPOTHILONE COMPOUNDS
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Page/Page column 30, (2008/06/13)
The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m-Z- wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.
Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide
Vlahov, Iontcho R.,Santhapuram, Hari Krishna R.,Kleindl, Paul J.,Howard, Stephen J.,Stanford, Katheryn M.,Leamon, Christopher P.
, p. 5093 - 5096 (2007/10/03)
An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described. EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, desacetylvinblastine monohydrazide. Both molecules are connected in re
