ChemInform Abstract: Synthesis of N-α-Aminoacyl Derivatives of Melphalan for Potential Use in Drug Targeting.

ChemInform ◽  
2010 ◽  
Vol 28 (5) ◽  
pp. no-no
Author(s):  
D. W. LARDEN ◽  
H. T. A. CHEUNG
Keyword(s):  
Drug Targeting ◽  
Derivatives Of ◽  
Potential Use

Synthesis of N-α-aminoacyl derivatives of melphalan for potential use in drug targeting

1996 ◽  
Vol 37 (42) ◽  
pp. 7581-7582 ◽  
Author(s):  
Dale W. Larden ◽  
H.T.Andrew Cheung
Keyword(s):  
Drug Targeting ◽  
Derivatives Of ◽  
Potential Use

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

β-Acarbose. I The Synthesis of 1-Epivalienamine

1997 ◽  
Vol 50 (3) ◽  
pp. 193 ◽  
Author(s):  
Joseph C. McAuliffe ◽  
Robert V. Stick
Keyword(s):  
Derivatives Of ◽  
Potential Use

Improvements and modifications to a literature procedure for the synthesis of multigram amounts of a derivative of 1-epivalienamine are described. As well, various other derivatives of 1-epivalienamine, of potential use in the synthesis of carba sugars, are reported.

Total synthesis of indole and dihydroindole alkaloids. X.1,2 The preparation of novel oxygenated catharanthine derivatives

1977 ◽  
Vol 55 (18) ◽  
pp. 3227-3234 ◽  
Author(s):  
James P. Kutney ◽  
Gordon H. Bokelman ◽  
Masahiro Ichikawa ◽  
Edwin Jahngen ◽  
Alummoottil V. Joshua ◽  
...  
Keyword(s):  
Double Bond ◽  
Total Synthesis ◽  
Osmium Tetroxide ◽  
Electrophilic Attack ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Potential Use

Detailed investigations involving the electrophilic attack of various reagents on the 3,4-double bond of catharanthine derivatives (e.g. 3, R = O) furnished a series of novel derivatives of potential use in the syntheses of naturally occurring bisindole alkaloids. These studies include such reagents as peracid, osmium tetroxide, and positive iodine.

scholarly journals GRP78 Protein Expression in Ovarian Cancer Patients and Perspectives for a Drug-Targeting Approach

2012 ◽  
Vol 2012 ◽  
pp. 1-5 ◽  
Author(s):  
Florence Delie ◽  
Patrick Petignat ◽  
Marie Cohen
Keyword(s):  
Ovarian Cancer ◽  
Drug Delivery ◽  
Drug Targeting ◽  
Drug Delivery Systems ◽  
Ovarian Cancer Cell ◽  
Glucose Deprivation ◽  
Chaperone Protein ◽  
Low Levels ◽  
Potential Use ◽  
Glucose Regulated Protein

Glucose-regulated protein of 78 kD (GRP78) is a chaperone protein mainly located in the endoplasmic reticulum (ER). This protein is normally present at low levels in adult cells but its expression is triggered by ER stress including glucose deprivation and hypoxia. In tumor cells, it is overexpressed with fraction of protein found at the cell surface. This paper presents the physiology of GRP78 in the context of ovarian cancer and its potential use as drug delivery systems targeting ovarian cancer cell.

SYNTHESIS OF 3-AMINO-2,3-DIDEOXY-D-lyxo-HEXOSE

1965 ◽  
Vol 43 (11) ◽  
pp. 3074-3079 ◽  
Author(s):  
Hans H. Baer ◽  
Frank Kienzle
Keyword(s):  
Aspartic Acid ◽  
Catalytic Hydrogenation ◽  
Title Compound ◽  
Amine Hydrochloride ◽  
Derivatives Of ◽  
Potential Use

Catalytic hydrogenation of methyl 4,6-O-benzylidene-2,3-dideoxy-3-nitro-β-D-threo-hexo-pyranos-2-enide (I) afforded methyl 4,6-O-benzylidene-2,3-dideoxy-3-nitro-β-D-lyxo-hexo-pyranoside (II). Acid debenzylidenation and further hydrogenation gave in turn methyl 2,3-dideoxy-3-nitro-β-D-lyxo-hexopyranoside (III) and the corresponding amine hydrochloride (IV). Several crystalline derivatives of IV were prepared, and the configuration at C-3 was proved by degradation of the N-benzoate (VII) to N-benzoyl-D-aspartic acid. The title compound (V) was obtained as a chromatographically homogeneous sirup.Some methyl 3-deoxy-3-nitro-β-L-hexopyranosides were prepared for potential use as starting materials in analogous syntheses in the L-series.

Properties and uses of neem, Azadirachta indica

1990 ◽  
Vol 68 (1) ◽  
pp. 1-11 ◽  
Author(s):  
Opender Koul ◽  
Murray B. Isman ◽  
C. M. Ketkar
Keyword(s):  
Azadirachta Indica ◽  
Third World ◽  
Agricultural Crops ◽  
Neem Tree ◽  
The Third ◽  
Economic Exploitation ◽  
Human Use ◽  
The Third World ◽  
Derivatives Of ◽  
Potential Use

The versatility of the neem tree Azadirachta indica A. Juss. is reviewed. This species, native to India, grows in nutrient-poor soils in arid habitats and has tremendous potential for human use. Various derivatives of the tree have potential use in toiletries, pharmaceuticals, the manufacture of agricultural implements and furniture, cattle and poultry feeds, nitrification of soils for various agricultural crops, and pest control. Since neem is a natural renewal resource producing extensive useful biomass, its propagation and economic exploitation will be beneficial, particularly to the Third World. In recent years, some useful commercial products have been developed from A. indica, and mere is considerable scope for future product development. Potentially profitable lines of research on this plant species are suggested.

scholarly journals Carboxy derivatives of isoflavones as affinity carriers for cytotoxic drug targeting in adrenocortical H295R carcinoma cells

2003 ◽  
Vol 179 (3) ◽  
pp. 395-403 ◽  
Author(s):  
D Somjen ◽  
N Stern ◽  
E Knoll ◽  
O Sharon ◽  
B Gayer ◽  
...  
Keyword(s):  
Drug Targeting ◽  
Specific Activity ◽  
Carcinoma Cells ◽  
Cytotoxic Drug ◽  
Biochanin A ◽  
Rat Tissues ◽  
Antagonist Activity ◽  
Wide Range ◽  
H295r Cells ◽  
Derivatives Of

Carboxy derivatives of isoflavones that exhibit oestrogenic/anti-oestrogenic properties were used as carriers for affinity drug targeting to H295R adrenocortical carcinoma cells that express transcripts of oestrogen receptor (ER) alpha and beta. These derivatives were prepared by introducing a carboxymethyl group at the 6-position of genistein and of biochanin A, yielding 6CG and 6CB respectively. In transactivation assays, 6CG displayed mixed agonist/antagonist activity for ERalpha, whereas 6CB displayed only weak antagonist activity. Low concentrations of oestrogen, 6CG and 6CB were capable of inducing proliferation in H295R cells and of stimulating creatine kinase (CK) specific activity, suggesting that these cells were sensitive to oestrogenic compounds. In in vivo experiments, both 6CG and 6CB were capable of inhibiting oestrogen-induced CK specific activity in rat tIssues. For affinity drug targeting, the cytotoxic drug daunomycin was coupled to 6CB and 6CG, yielding 6CB-Dau and 6CG-Dau respectively. These conjugates were tested for their antiproliferative ability to inhibit DNA synthesis as assessed by incorporation of [(3)H]thymidine in H295R cells. A dose-dependent cytoxicity was observed with both conjugates. At 0.3-3 nM, both conjugates were 10 to 30 times more potent than daunomycin. At 30 nM these conjugates were two to three times more potent than daunomycin. At concentrations ranging between 300 and 3000 nM, no difference in cytotoxicity was observed between the conjugates and daunomycin. When the cells were treated over a wide range of concentrations with a combination of 6CG plus daunomycin, the observed cytotoxicity was less than with daunomycin alone. When non-transformed rat enterocytes, which do not express ER, were treated with 6CG-Dau or daunomycin, the antiproliferative effect of 6CG-Dau was the same as that of daunomycin over the concentration range tested. These pilot studies suggest that the ready availability of oestrogenic binding sites in H295R cells can be exploited for site-directed chemotherapy.

scholarly journals Investigations of Azulene Derivatives as Self-Indicating Chromophores for Applications in Protecting Group Strategies and Solid-Phase Purification

2021 ◽  
Author(s):  
◽  
Thomas Bevan
Keyword(s):  
Electronic Properties ◽  
Solid Phase ◽  
Protecting Groups ◽  
Protecting Group ◽  
Blue Colour ◽  
Derivatives Of ◽  
Potential Use

<p>Azulene is a hydrocarbon that exhibits an intense blue colour. Derivatives of azulene exhibit different colours depending on the position and electronic properties of the substituents. The chemical and chromophoric properties of azulene and guaiazulene derivatives are investigated for the potential use in applications such as chromophoric protecting groups and self-indicating scavenger resins. Investigations were carried out on the scope of known reactions on the 3- position of guaiazulene for this purpose...</p>

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