Advances in the development of hybrid anticancer drugs

Enhancement of the cytotoxic potential of the mixed EGFR and DNA-targeting ‘combi-molecule’ ZRBA1 against human solid tumour cells by a bis-quinazoline-based drug design approach

(2012) Sherin Al-Safadi et al.   ANTI-CANCER DRUGS

Targeting the Estrogen Receptor using Steroid–Therapeutic Drug Conjugates (Hybrids)

(2012) Kinh-Luan Dao et al.   BIOCONJUGATE CHEMISTRY

Biological Effects of AL622, a Molecule Rationally Designed to Release an EGFR and a c-Src Kinase Inhibitor

(2012) Anne-Laure Larroque-Lombard et al.   Chemical Biology & Drug Design

Synthetically Accessible Non-Secosteroidal Hybrid Molecules Combining Vitamin D Receptor Agonism and Histone Deacetylase Inhibition

(2012) Joshua Fischer et al.   CHEMISTRY & BIOLOGY

Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil–isatin conjugates and their cytotoxic evaluation

(2012) Kewal Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Azide-alkyne cycloaddition en route to novel 1H-1,2,3-triazole tethered isatin conjugates with in vitro cytotoxic evaluation

(2012) Pardeep Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and anticancer activity of nitric oxide donating/chalcone hybrids

(2012) Mai A.E. Mourad et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

“Combi-targeting” mitozolomide: Conferring novel signaling inhibitory properties to an abandoned DNA alkylating agent in the treatment of advanced prostate cancer

(2012) Youqiang Fang et al.   PROSTATE

Design, synthesis, cytocidal activity and estrogen receptor α affinity of doxorubicin conjugates at 16α-position of estrogen for site-specific treatment of estrogen receptor positive breast cancer

(2012) Pijus Saha et al.   STEROIDS

Synthesis and Anticancer Activity of Isatin-Based Pyrazolines and Thiazolidines Conjugates

(2011) Dmytro Havrylyuk et al.   ARCHIV DER PHARMAZIE

The Application of Tandem Aza-Wittig Reaction to Synthesize Artemisinin-Guanidine Hybrids and Their Anti-Tumor Activity

(2011) Lijun Xie et al.   ARCHIV DER PHARMAZIE

Cytotoxicity and cell death mechanisms induced by the polyamine-vectorized anti-cancer drug F14512 targeting topoisomerase II

(2011) Viviane Brel et al.   BIOCHEMICAL PHARMACOLOGY

Hybrid compounds as new Bcr/Abl inhibitors

(2011) Deping Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, characterization and anticancer studies of mixed ligand dithiocarbamate palladium(II) complexes

(2011) Hizbullah Khan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

1,2,3-Triazole tethered β-lactam-Chalcone bifunctional hybrids: Synthesis and anticancer evaluation

(2011) Pardeep Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, antiproliferative activity and estrogen receptor α affinity of novel estradiol-linked platinum(II) complex analogs to carboplatin and oxaliplatin. Potential vector complexes to target estrogen-dependent tissues

(2011) Pijus Saha et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Quaternary ammonium-melphalan conjugate for anticancer therapy of chondrosarcoma: in vitro and in vivo preclinical studies

(2011) Caroline Peyrode et al.   INVESTIGATIONAL NEW DRUGS

Synthesis and cytotoxicity studies of bifunctional hybrids of nitrogen mustards with potential enzymes inhibitors based on melamine framework

(2011) Beata Kolesinska et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

A bioanalytical investigation on the exquisitely strong in vitro potency of the EGFR–DNA targeting type II combi-molecule ZR2003 and its mitigated in vivo antitumour activity

(2011) Nahid Golabi et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

MGMT Is a Molecular Determinant for Potency of the DNA-EGFR-Combi-Molecule ZRS1

(2011) Y. Huang et al.   MOLECULAR CANCER RESEARCH

Design of novel tyrosine-nitrogen mustard hybrid molecules active against uterine, ovarian and breast cancer cell lines

(2011) Caroline Descôteaux et al.   STEROIDS

Inhibition of DNA Synthesis by a Platinum–Acridine Hybrid Agent Leads to Potent Cell Kill in Nonsmall Cell Lung Cancer

(2011) Christopher L. Smyre et al.   ACS Medicinal Chemistry Letters

Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids

(2010) Marc Lamblin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and anticancer activities of stilbene-coumarin hybrid compounds: Identification of novel proapoptotic agents

(2010) Federica Belluti et al.   BIOORGANIC & MEDICINAL CHEMISTRY

First synthesis of separable isomeric testosterone dimers showing differential activities on prostate cancer cells

(2010) Dominic Bastien et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of retinoid-chalcones as inhibitors of colon cancer cell growth

(2010) Cassia S. Mizuno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and in vitro evaluation of novel coumarin–chalcone hybrids as potential anticancer agents

(2010) Koneni V. Sashidhara et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The combi-targeting concept: Mechanism of action of the pleiotropic combi-molecule RB24 and discovery of a novel cell signaling-based combination principle

(2010) Ranjita Banerjee et al.   CELLULAR SIGNALLING

Synthesis and docking studies of novel benzopyran-2-ones with anticancer activity

(2010) Magda M.F. Ismail et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and cytotoxicity evaluation of (tetrahydro-β-carboline)-1,3,5-triazine hybrids as anticancer agents

(2010) Ravi Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents

(2010) Ahmed Kamal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Physical Properties, and Cytotoxicity of Nitroxyl-Aziridine Hybrid

(2010) Takuya Kumamoto et al.   HELVETICA CHIMICA ACTA

Characterization of the potency of epidermal growth factor (EGFR)-DNA targeting combi-molecules containing a hydrolabile carbamate at the 3-position of the triazene chain

(2010) Meaghan MacPhee et al.   INVESTIGATIONAL NEW DRUGS

Evaluation of new iodinated acridine derivatives for targeted radionuclide therapy of melanoma using 125I, an Auger electron emitter

(2010) Maryline Gardette et al.   INVESTIGATIONAL NEW DRUGS

Biosynthesis, synthesis, and biological activities of pyrrolobenzodiazepines

(2010) Barbara Gerratana   MEDICINAL RESEARCH REVIEWS

Hybrid anticancer agents: Isothiocyanate–progesterone conjugates as chemotherapeutic agents and insights into their cytotoxicities

(2009) Shreelekha Adsule et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Total synthesis of a library of designed hybrids of the microtubule-stabilising anticancer agents taxol, discodermolide and dictyostatin

(2009) Ian Paterson et al.   CHEMICAL COMMUNICATIONS

Design, Synthesis, and Biological Evaluation of Artificial Macrosphelides in the Search for New Apoptosis-Inducing Agents

(2009) Yuji Matsuya et al.   CHEMISTRY-A EUROPEAN JOURNAL

VP-128, a novel oestradiol-platinum(II) hybrid with selective anti-tumour activity towards hormone-dependent breast cancer cells in vivo

(2009) Céline Van Themsche et al.   ENDOCRINE-RELATED CANCER

Promise and challenges in drug discovery and development of hybrid anticancer drugs

(2009) Lalji K Gediya et al.   Expert Opinion on Drug Discovery

Preclinical investigation of tolerance and antitumour activity of new fluorodeoxyglucose-coupled chlorambucil alkylating agents

(2009) Elisabeth Miot-Noirault et al.   INVESTIGATIONAL NEW DRUGS

Preclinical activity of F14512, designed to target tumors expressing an active polyamine transport system

(2009) Anna Kruczynski et al.   INVESTIGATIONAL NEW DRUGS

AntitumorPsoropermumXanthones andSarcomelicopeAcridones: Privileged Structures Implied in DNA Alkylation†

(2009) Hung The Nguyen et al.   JOURNAL OF NATURAL PRODUCTS

Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma

(2008) Nicolas Desbois et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents

(2008) L. Guandalini et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

F14512, a Potent Antitumor Agent Targeting Topoisomerase II Vectored into Cancer Cells via the Polyamine Transport System

(2008) J.-M. Barret et al.   CANCER RESEARCH

Total synthesis of a potent hybrid of the anticancer natural products dictyostatin and discodermolide

(2008) Ian Paterson et al.   CHEMICAL COMMUNICATIONS

Mechanism of apoptosis induced by a newly synthesized derivative of macrosphelides with a thiazole side chain

(2008) Kanwal Ahmed et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Evaluation of Radiolabeled (Hetero)Aromatic Analogues ofN-(2-diethylaminoethyl)-4-iodobenzamide for Imaging and Targeted Radionuclide Therapy of Melanoma

(2008) Jean-Michel Chezal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of practical syntheses of the marine anticancer agents discodermolide and dictyostatin

(2008) Gordon J. Florence et al.   NATURAL PRODUCT REPORTS

Incorporation of histone deacetylase inhibition into the structure of a nuclear receptor agonist

(2008) L. E. Tavera-Mendoza et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Improved synthesis of unique estradiol-linked platinum(II) complexes showing potent cytocidal activity and affinity for the estrogen receptor alpha and beta

(2008) Caroline Descôteaux et al.   STEROIDS

Hybrid Molecules with a Dual Mode of Action: Dream or Reality?†

(2007) Bernard Meunier   ACCOUNTS OF CHEMICAL RESEARCH